Waleffe A, Guillaume D, Mary-Rabine L, Kulbertus H
Acta Cardiol. 1980;35(4):257-68.
Moxaprindine, a new derivative of aprindine, has been showed to possess strong antiarrhythmic properties in the dog. It is significantly less toxic than aprindine on hematopoietic cells in culture. This drug was given intravenously (2 mg/kg given over a 30 min period), to 10 patients with severe, refractory and symptomatic ventricular arrhythmias. In 8 of them, all ventricular ectopic activity was suppressed for at least 90 min following the end of perfusion. In 7, no ventricular ectopic beats recurred before the end of the experimentation (150 min). There were two non-responders: one of them developed a torsade de pointes phenomenon under the influence of the drug. The mean drug concentration which was reached at the end of perfusion was 4.83 +/- 2.46 gamma/ml. It progressively fell to a value of 1.11 +/- 0.35 gamma/ml, 150 min later. The drug prolongs the PR interval, QRS duration and QT interval. Moxaprindine is a powerful antiarrhythmic agent which deserves further assessment in long term studies.
莫沙丙啶是阿普林定的一种新衍生物，已证明在犬身上具有很强的抗心律失常特性。在培养的造血细胞上，它的毒性明显低于阿普林定。该药物以静脉注射方式（在30分钟内给予2毫克/千克）给予10例患有严重、难治性且有症状的室性心律失常患者。其中8例，在灌注结束后至少90分钟内所有室性异位活动均受到抑制。7例在实验结束前（150分钟）未再出现室性异位搏动。有2例无反应者：其中1例在药物影响下出现尖端扭转型室速现象。灌注结束时达到的平均药物浓度为4.83±2.46微克/毫升。150分钟后逐渐降至1.11±0.35微克/毫升。该药物可延长PR间期、QRS时限和QT间期。莫沙丙啶是一种强效抗心律失常药物，值得在长期研究中进一步评估。
